Vepdegestrant-d5
Vepdegestrant-d5 (ARV-471-d5) is the deuterium labeled Vepdegestrant (HY-138642). Vepdegestrant (ARV-471) is an orally active PROTAC estrogen receptor degrader against breast cancer. Vepdegestrant is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase complex. Vepdegestrant leads to the ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. Vepdegestrant robustly degrades ER in ER-positive breast cancer cell lines with a DC50 of about 2 nM.
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- CAS. Nr.: 3025452-07-4
- Formel: C45H44D5N5O4
- Molecular Weight:728.93
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
Beschreibung
In Vitro
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Anwendung
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
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CAS. Nr. 3025452-07-4
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Unlabeled CAS 2229711-68-4
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Molecular Weight 728.93
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Formel C45H44D5N5O4
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SMILES
O=C1NC([C@@H](N(C2=O)CC3=C2C=CC(N(CC4)CCN4CC(CC5)CCN5C(C=C6)=CC=C6[C@H]7[C@@H](C8=C([2H])C([2H])=C([2H])C([2H])=C8[2H])CCC9=C7C=CC(O)=C9)=C3)CC1)=O
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Synonyms
ARV-471-d5 PF-07850327-d5
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
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Topics Targeted Protein Degradation (TPD): From PROTACs to Molecular Glues
Targeted protein degradation is a drug discovery strategy that uses cellular protein degradation systems to selectively eliminate disease-associated proteins, and its core modalities include PROTACs and molecular glue degraders.
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Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)